Target Information
| Target General Information | Top | |||||
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| Target ID |
T66903
(Former ID: TTDR00829)
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| Target Name |
Fascin (FSCN1)
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| Synonyms |
Singed-like protein; SNL; HSN; FAN1; 55 kDa actin-bundling protein; 55 kDa actin bundling protein
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| Gene Name |
FSCN1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Plays a role in the organization of actin filament bundles and the formation of microspikes, membrane ruffles, and stress fibers. Important for the formation of a diverse set of cell protrusions, such as filopodia, and for cell motility and migration. Organizes filamentous actin into bundles with a minimum of 4. 1:1 actin/fascin ratio.
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| UniProt ID | ||||||
| Sequence |
MTANGTAEAVQIQFGLINCGNKYLTAEAFGFKVNASASSLKKKQIWTLEQPPDEAGSAAV
CLRSHLGRYLAADKDGNVTCEREVPGPDCRFLIVAHDDGRWSLQSEAHRRYFGGTEDRLS CFAQTVSPAEKWSVHIAMHPQVNIYSVTRKRYAHLSARPADEIAVDRDVPWGVDSLITLA FQDQRYSVQTADHRFLRHDGRLVARPEPATGYTLEFRSGKVAFRDCEGRYLAPSGPSGTL KAGKATKVGKDELFALEQSCAQVVLQAANERNVSTRQGMDLSANQDEETDQETFQLEIDR DTKKCAFRTHTGKYWTLTATGGVQSTASSKNASCYFDIEWRDRRITLRASNGKFVTSKKN GQLAASVETAGDSELFLMKLINRPIIVFRGEHGFIGCRKVTGTLDANRSSYDVFQLEFND GAYNIKDSTGKYWTVGSDSAVTSSGDTPVDFFFEFCDYNKVAIKVGGRYLKGDHAGVLKA SAETVDPASLWEY Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T89GNB | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | NP-G2-044 | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | NP-G2-044 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: 5-[(3,4-dichlorophenyl)methyl]-4-oxo-1-piperidin-4-yl-N-pyridin-4-ylpyrazolo[4,3-c]pyridine-7-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF FASCIN IN COMPLEX WITH BDP-13176 | PDB:6I18 | ||||
| Method | X-ray diffraction | Resolution | 1.49 Å | Mutation | No | [2] |
| PDB Sequence |
VQIQFGLINC
19 GNKYLTAEAF29 GFKVNASASS39 LKKKQIWTLE49 QPPDEAGSAA59 VCLRSHLGRY 69 LAADKDGNVT79 CEREVPGPDC89 RFLIVAHDDG99 RWSLQSEAHR109 RYFGGTEDRL 119 SCFAQTVSPA129 EKWSVHIAMH139 PQVNIYSVTR149 KRYAHLSARP159 ADEIAVDRDV 169 PWGVDSLITL179 AFQDQRYSVQ189 TADHRFLRHD199 GRLVARPEPA209 TGYTLEFRSG 219 KVAFRDCEGR229 YLAPSGPSGT239 LKAGKATKVG249 KDELFALEQS259 CAQVVLQAAN 269 ERNVSTRQGM279 DLSANQDEET289 DQETFQLEID299 RDTKKCAFRT309 HTGKYWTLTA 319 TGGVQSTASS329 KNASCYFDIE339 WRDRRITLRA349 SNGKFVTSKK359 NGQLAASVET 369 AGDSELFLMK379 LINRPIIVFR389 GEHGFIGCRK399 VTGTLDANRS409 SYDVFQLEFN 419 DGAYNIKDST429 GKYWTVGSDS439 AVTSSGDTPV449 DFFFEFCDYN459 KVAIKVGGRY 469 LKGDHAGVLK479 ASAETVDPAS489 LWEY
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| Ligand Name: 2-[(3,4-dichlorophenyl)methyl]-~{N}-(1-methylpyrazol-4-yl)-1-oxidanylidene-6-piperidin-4-yl-2,7-naphthyridine-4-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF FASCIN IN COMPLEX WITH COMPOUND 24 | PDB:6I17 | ||||
| Method | X-ray diffraction | Resolution | 1.56 Å | Mutation | No | [2] |
| PDB Sequence |
VQIQFGLINC
19 GNKYLTAEAF29 GFKVNASASS39 LKKKQIWTLE49 QPPDEAGSAA59 VCLRSHLGRY 69 LAADKDGNVT79 CEREVPGPDC89 RFLIVAHDDG99 RWSLQSEAHR109 RYFGGTEDRL 119 SCFAQTVSPA129 EKWSVHIAMH139 PQVNIYSVTR149 KRYAHLSARP159 ADEIAVDRDV 169 PWGVDSLITL179 AFQDQRYSVQ189 TADHRFLRHD199 GRLVARPEPA209 TGYTLEFRSG 219 KVAFRDCEGR229 YLAPSGPSGT239 LKAGKATKVG249 KDELFALEQS259 CAQVVLQAAN 269 ERNVSTRQGM279 DLSANQDEET289 DQETFQLEID299 RDTKKCAFRT309 HTGKYWTLTA 319 TGGVQSTASS329 KNASCYFDIE339 WRDRRITLRA349 SNGKFVTSKK359 NGQLAASVET 369 AGDSELFLMK379 LINRPIIVFR389 GEHGFIGCRK399 VTGTLDANRS409 SYDVFQLEFN 419 DGAYNIKDST429 GKYWTVGSDS439 AVTSSGDTPV449 DFFFEFCDYN459 KVAIKVGGRY 469 LKGDHAGVLK479 ASAETVDPAS489 LWEY
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 2.23E-01 | Radiality | 1.39E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.09E+02 | Topological coefficient | 1.00E+00 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents. Bioorg Med Chem Lett. 2019 Apr 15;29(8):1023-1029. | |||||
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